LY2157299 is a selective inhibitor of the transforming growth factor-beta (TGF-β) receptor type I kinase. It has been primarily investigated for its potential in cancer therapy, particularly due to its ability to block the TGF-β signaling pathway, which plays a key role in tumor progression, metastasis, and immune evasion. By inhibiting this pathway, LY2157299 can help suppress tumor growth and enhance the body’s immune response against cancer cells.

It has been studied in clinical trials for various solid tumors, including glioblastoma, pancreatic cancer, and hepatocellular carcinoma. In combination with other therapies such as chemotherapy or immunotherapy, LY2157299 shows promise in improving treatment outcomes by targeting the tumor microenvironment and reducing fibrosis, which can improve drug delivery.

Additionally, due to its anti-fibrotic properties, it has been explored in non-oncological conditions involving tissue fibrosis, such as liver, kidney, and lung fibrosis, where abnormal TGF-β activation contributes to disease progression.